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Assay Detail

CHEMBL677169

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
50% inhibition of human recombinant fibroblast collagenase (MMP-1, HFC)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Interstitial collagenase (CHEMBL332)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibition of Matrix Metalloproteinases: An examination of the S1 pocket
Miller A, Askew M, Beckett R, Bellamy CL, Bone EA, Coates RE, Davidson AH, Drummond AH, Huxley P, Martin FM, Saroglou L, Thompson AJ, van Dijk SE, Whittaker M
Bioorg Med Chem Lett (1997) 7 : 193 -198
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.03 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279786 BATIMASTAT 2.0 1 8.30
CHEMBL279785 MARIMASTAT 3.0 1 8.30
CHEMBL58945 1 7.70
CHEMBL60546 1 7.70
CHEMBL294066 1 6.82
CHEMBL62245 1 6.40
CHEMBL62056 1 6.30
CHEMBL293382 1 6.00
CHEMBL58997 1 5.30
CHEMBL416510 1 5.16
CHEMBL59185 1 5.16
CHEMBL292160 1 5.10
CHEMBL62186 1 4.70
CHEMBL418472 1 4.70
CHEMBL61538 1 4.52
CHEMBL59722 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279786 BATIMASTAT IC50 = 5.0 nM 8.30
CHEMBL279785 MARIMASTAT IC50 = 5.0 nM 8.30
CHEMBL58945 IC50 = 20.0 nM 7.70
CHEMBL60546 IC50 = 20.0 nM 7.70
CHEMBL294066 IC50 = 150.0 nM 6.82
CHEMBL62245 IC50 = 400.0 nM 6.40
CHEMBL62056 IC50 = 500.0 nM 6.30
CHEMBL293382 IC50 = 1000.0 nM 6.00
CHEMBL58997 IC50 = 5000.0 nM 5.30
CHEMBL416510 IC50 = 7000.0 nM 5.16
CHEMBL59185 IC50 = 7000.0 nM 5.16
CHEMBL292160 IC50 = 8000.0 nM 5.10
CHEMBL62186 IC50 = 20000.0 nM 4.70
CHEMBL418472 IC50 = 20000.0 nM 4.70
CHEMBL61538 IC50 = 30000.0 nM 4.52
CHEMBL59722 IC50 = 50000.0 nM 4.30